Why are some NSAIDs known as 'Traditional'?
They only block one COX
The block both COXs
Describe COX1
Constituative
Inducible
Membrane bound
Cytoplasmic
The channels of both COX1 & COX 2 are constricted to prevent incorrect substrate binding
Where do NSAIDs bind on COX 1?
Arg 120
Arg 130
Arg 140
Aspirin binds permenantly to the Ser 530 of COX1
Why does COX2 have a much wider channel than COX 1?
Val533 forces the channel to be wider
Ser533 forces the channel to be wider
Ile533 forces the channel to be wider
COX2 is inducible
The smaller channel of COX2 can be used for selective inhibition- i.e. Colecoxib
COX2 is much less responsible for inflammation than COX1
Why are selective COX2 inhibitors used on patients with G.I troubles?
They also repair mucus membranes
They have fewer side effects
They cannot be digested properly by healthy tracts
What is the most common side effect of NSAIDs?
GI troubles
Renal insufficiency
C.V disorders
Aspirin is the only NSAID thought not to cause cardiovascular disorders
Name the two NSAID side effects that contribute to cardiovascular disorders
Inc salt and water retention
Constant vasoconstriction effect endothelium
Cole/Paracoxib are traditional NSAIDs
What is the effect of Aspirin in platelets?
Reduced Thromboxin A2
Reduced Thromboxin I2
Reduced Thromboxin E2
The binding of aspirin lasts for the entire life of the platelet
To whom can Aspirin not be given?
Over 65s
Pregnant women
Children under 16
Paracetamol is anti-inflammatory but not antipyretic
The action of paracetamol is unknown
Why is paracetamol toxic to the liver in high doses?
Oversaturates the removal pathway
Causing an alternative to be used
The alternative paracetamol removal pathway causes an increase in toxic NAPQ1
